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Synthesis And Anticancer Evaluation Of Furoquinoline Derivatives | 8274
ISSN: 0975-0851

Journal of Bioequivalence & Bioavailability
Open Access

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Synthesis and anticancer evaluation of Furoquinoline derivatives

2nd World Congress on Bioavailability & Bioequivalence: Pharmaceutical R & D Summit-2011 and International Conference on Pharmaceutics & Novel Drug Delivery Systems

Cherng-Chyi Tzeng, Yu-Wen Chen, and Yeh-Long Chen

Special Issue BABE-2011: Posters: JBB

DOI: 10.4172/0975-0851.1000105

Abstract
C ertain 4-anilinofuro[2,3- b ]quinoline derivatives were synthesized and evaluated for their anticancer activities against human cervical epithelioid carcinoma (HeLa), hepatocelluar carcinoma (SKHep1), oral squamous cell carcinoma (SAS), human stomach adenocarcinoma (AGS), non-small cell lung cancer (A549), and esophageal carcinoma (CE81T). Among these compounds tested, 1-[4-(furo[2,3- b ] quinolin-4-ylamino)phenyl]ethanone ( 1 ) was the most potent with mean GI 50 values of less than 4.2 micromole respectively against the growth of HeLa, SKHep, and CE81T cells and therefore, was further evaluated on its eff ects of cell cycle distribution. Results indicated that lead compound 1 induces cell cycle arrest in G2/M followed by apoptosis. However, some drawbacks such as lack of selective cytotoxicity, poor oral bioavailability, and poor water solubility exhibited by 1 prompted us to search for newer derivatives with better pharmacokinetic profi les and higher water solubility. Various aminoalkoxyimino derivatives of 1 have been synthesized and evaluated. Some of them exhibited selective anticancer activity against the growth of non-small cell lung cancers (especially NCI-H460) and higher water solubility than the lead compound. Xenograghic studies and orthotropic lung cancer model in nude mice using H1229 cells indicated that certain aminoalkoxyimino derivatives of 1 exhibited signifi cant effi cacy in inhibiting tumor growth in vivo . Further structural optimization and mechanism studies are on-going.
Biography
Dr. Cherng-Chyi Tzeng has completed his Ph. D degree from the University of Rhode Island, USA in 1984. He is the Dean of General Affairs at Kaohsiung Medical University, Taiwan. He has published more than 120 papers in reputed journals and serving as an editorial board member of Kaohsiung Journal of Medical Sciences (SCI Journal).
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